PURPOSE: To provide a new cyclophane which has the blood pressure lowering activity, coronary blood vessels dilating activity, and heartbeat rate lowering activity, and is effectively used in the therapy of hypertension and ischemic heart disease.
CONSTITUTION: This compound is represented by formula I [X1 and X2 are each 2-4C alkylene or alkenylene; A is 1-6C alkylene, -Y1-A1-, (Y1 is O, sulfhenyl or the like; A is 2-4C alkylene) or the like; R1-R4 are each H, halogen, 1-3C alkyl, hydroxyl or the like; R is cyano, general formula II (R5 is H, 1-10C alkyl or the like; R6 is H, 1-5C alkyl, or the like) or the like], e.g. 4-(3-piperidin-1-yl) prop-1-yl)-[2,2] paracyclophane. The compound is prepared by reacting a compound of formula III (Z1 is halogen, nucleophilic residue) with amine of the formula H-R, or an alkali metal salt thereof in a solvent such as THF or the like, optionally in the presence of an acid binder (e.g. triethylamine) at a temp. of 0-100°C.
FUORUKERU TORATSUHA
